FG 7142 (ZK 39106; LSU-65), a non-specificly benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.
Physicochemical Properties
| Molecular Formula | C13H11N3O |
| Molecular Weight | 225.24594 |
| Exact Mass | 225.09 |
| Elemental Analysis | C, 69.32; H, 4.92; N, 18.66; O, 7.10 |
| CAS # | 78538-74-6 |
| PubChem CID | 4375 |
| Appearance | Light yellow to yellow solid powder |
| Density | 1.328g/cm3 |
| Boiling Point | 576.3ºC at 760 mmHg |
| Flash Point | 302.3ºC |
| Index of Refraction | 1.735 |
| LogP | 2.466 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 2 |
| Rotatable Bond Count | 1 |
| Heavy Atom Count | 17 |
| Complexity | 307 |
| Defined Atom Stereocenter Count | 0 |
| SMILES | CNC(=O)C1=NC=C2C(=C1)C3=CC=CC=C3N2 |
| InChi Key | QMCOPDWHWYSJSA-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C13H11N3O/c1-14-13(17)11-6-9-8-4-2-3-5-10(8)16-12(9)7-15-11/h2-7,16H,1H3,(H,14,17) |
| Chemical Name | N-methyl-9H-pyrido[3,4-b]indole-3-carboxamide |
| Synonyms | FG-7142 FG 7142 FG7142 |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vitro | FG-7142 exhibits affinity for α subunit expression, with a Ki value of 91 nM; 330 nm; α1, α2, α3, and α5 subunits, respectively, being 492 nM and 2.150 μM[1]. When it comes to controlling GABA-induced chloride flux at GABAA receptors that express the α1 subunit energy (EC50 = 137 nM) micron), FG-7142 is much more effective than other α subunits (EC50: α2=507 nM, α3=1.021μM, and α5=1.439) [1]. |
| ln Vivo | In rats, FG-7142 (ip; 15–30 mg/kg) increases dopamine in the nucleus accumbens and prefrontal cortex by activating mesolimbic cortical dopaminergic projections [1]. In vivo, FG-7142 (ip; 15 mg/kg) raises dopamine turnover and tyrosine hydroxylase activity in the ventral tegmentum and medial prefrontal cortex, but not in the mesolimbic or nigrostriatal regions [1]. |
| References |
[1]. FG 7142 specifically reduces meal size and the rate and regularity of sustained feeding in female rats: evidence that benzodiazepine inverse agonists reduce food palatability.Neuropsychopharmacology. 2007 May;32(5):1069-81. Epub 2006 Nov. |
| Additional Infomation | N-methyl-9H-pyrido[3,4-b]indole-3-carboxamide is a member of beta-carbolines. |
Solubility Data
| Solubility (In Vitro) | DMSO : ~100 mg/mL (~443.95 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (11.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4395 mL | 22.1976 mL | 44.3951 mL | |
| 5 mM | 0.8879 mL | 4.4395 mL | 8.8790 mL | |
| 10 mM | 0.4440 mL | 2.2198 mL | 4.4395 mL |